Indian Patents. 268804:"AMINOPHOSPHONIC ACID DERIVATIVES, ADDITION SALTS THEREOF AND S1P RECEPTOR MODULATORS"

Title of Invention	"AMINOPHOSPHONIC ACID DERIVATIVES, ADDITION SALTS THEREOF AND S1P RECEPTOR MODULATORS"
Abstract	Aminophosphonic acid derivatives represented by the general formula (1) (such as 2-amino-5-[4-(3-benzyloxyphenyl-thio)-2-chlorophenyl]-2-methylpentylphosphonic acid mono-esters) exhibit excellent modulatory activity on S1P receptor and are reduced in adverse reaction.

Full Text	we Claims 1. An SIP receptor modulator containing as an active ngredient at least one of aminophosphonic acid derivatives represented by the following general formula (1): (Formula Removed) [wherein Ri is a hydrogen atom, a halogen atom, a halogenated or unhalogenated lower alkyl group having 1 to 4 carbon atoms, a hydroxy group, a phenyl group, an aralkyl group, a lower alkoxy group having 1 to 4 carbon atoms, a trifluoromethyloxy group, a substituted or unsubstituted phenoxy group, a cyclohexylmethyloxy group, a substituted or unsubstituted aralkyloxy group, a pyridylmethyloxy group, a cinnamyloxy group, a naphthylmethyloxy group, a phenoxymethyl group, a hydroxymethyl group, a hydroxyethyl group, a lower alkylthio group having 1 to 4 carbon atoms, a lower alkylsulfinyl group having 1 to 4 carbon atoms, a lower alkylsulfonyl group having 1 to 4 carbon atoms, a benzylthio group, an acetyl group, a nitro group or a cyano group; R2 is a hydrogen atom, a halogen atom, a halogenated or unhalogenated lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, an aralkyl group or an aralkyloxy group; R3 is a hydrogen atom, a halogen atom, a trifluoromethyl group, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, a hydroxy group, a benzyloxy group, a phenyl group, a lower alkoxymethyl group having 1 to 4 carbon atoms or a lower alkylthio group having 1 to 4 carbon atoms; R4 is a hydrogen atom, a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxymethyl group having 1 to 4 carbon atoms, a lower alkylthiomethyl group having 1 to 4 carbon atoms, a hydroxymethyl group, a phenyl group or an aralkyl group; R5 is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; X is 0, S, SO or S02; Y is -CH2O-, -CH2-, -CH=CH-, -CH=CF-, -CH2CH2-, -CH2CFH-, -CH2CF2-or -CH(OH)CF2-; and n is an integer from 1 to 4], and optical isomers, and pharmaceutically acceptable salts and hydrates thereof. 2. The SIP receptor modulator according to claim A, wherein the compound represented by the general formula (1) contains as an active ingredient at least one of 2-aminophosphonic acid monoester derivatives represented by the following general formula (la): (Formula Removed) [wherein R3, R4, X and n are as defined above], and the optical isomers, the pharmaceutically acceptable salts and the hydrates thereof. 3. The SIP receptor modulator according to claim jj., wherein the compound represented by the general formula (1) contains as an active ingredient at least one of 2-aminophosphonic acid derivatives represented by the following general formula (lb): (Formula Removed) [wherein R3, R4, X, Z and n are as defined above], and the optical isomers, the pharmaceutically acceptable salts and the hydrates thereof. 4. A pharmaceutical agent containing as an active ingredient at least one of the aminophosphonic acid derivatives according to any one of claims 1 to3, and the optical isomers, the pharmaceutically acceptable salts and the hydrates thereof.

Full Text

we Claims
1. An SIP receptor modulator containing as an active
ngredient at least one of aminophosphonic acid derivatives represented by the following general formula (1):
(Formula Removed)
[wherein Ri is a hydrogen atom, a halogen atom, a halogenated or unhalogenated lower alkyl group having 1 to 4 carbon atoms, a hydroxy group, a phenyl group, an aralkyl group, a lower alkoxy group having 1 to 4 carbon atoms, a trifluoromethyloxy group, a substituted or unsubstituted phenoxy group, a cyclohexylmethyloxy group, a substituted or unsubstituted
aralkyloxy group, a pyridylmethyloxy group, a cinnamyloxy group, a naphthylmethyloxy group, a phenoxymethyl group, a hydroxymethyl group, a hydroxyethyl group, a lower alkylthio group having 1 to 4 carbon atoms, a lower alkylsulfinyl group having 1 to 4 carbon atoms, a lower alkylsulfonyl group having 1 to 4 carbon atoms, a benzylthio group, an acetyl group, a nitro group or a cyano group; R2 is a hydrogen atom, a halogen atom, a halogenated or unhalogenated lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, an aralkyl group or an aralkyloxy group; R3 is a hydrogen atom, a halogen atom, a trifluoromethyl group, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, a hydroxy group, a benzyloxy group, a phenyl group, a lower alkoxymethyl group having 1 to 4 carbon atoms or a lower alkylthio group having 1 to 4 carbon atoms; R4 is a hydrogen atom, a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxymethyl group having 1 to 4 carbon atoms, a lower alkylthiomethyl group having 1 to 4 carbon atoms, a hydroxymethyl group, a phenyl group or an aralkyl group; R5 is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; X is 0, S, SO or S02; Y is -CH2O-, -CH2-, -CH=CH-, -CH=CF-, -CH2CH2-, -CH2CFH-, -CH2CF2-or -CH(OH)CF2-; and n is an integer from 1 to 4], and optical isomers, and pharmaceutically acceptable salts and hydrates thereof.
2. The SIP receptor modulator according to claim A, wherein the compound represented by the general formula (1) contains as an active ingredient at least one of 2-aminophosphonic acid monoester derivatives represented by the following general formula (la):
(Formula Removed)
[wherein R3, R4, X and n are as defined above], and the optical isomers, the pharmaceutically acceptable salts and the hydrates thereof.
3. The SIP receptor modulator according to claim jj., wherein
the compound represented by the general formula (1) contains as an active ingredient at least one of 2-aminophosphonic acid derivatives represented by the following general formula (lb):
(Formula Removed)
[wherein R3, R4, X, Z and n are as defined above], and the
optical isomers, the pharmaceutically acceptable salts and the
hydrates thereof.

4. A pharmaceutical agent containing as an active ingredient at least one of the aminophosphonic acid derivatives according to any one of claims 1 to3, and the optical isomers, the pharmaceutically acceptable salts and the hydrates thereof.

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Patent Number

268804

Indian Patent Application Number

2339/DELNP/2009

PG Journal Number

38/2015

Publication Date

18-Sep-2015

Grant Date

17-Sep-2015

Date of Filing

09-Apr-2009

Name of Patentee

KYORIN PHARMACEUTICAL CO., LTD.

Applicant Address

5, KANDA SURUGADAI 2-CHOME, CHIYODA-KU, TOKYO 101-8311 JAPAN.

Inventors:

#	Inventor's Name	Inventor's Address
1	KOHNO YASUSHI	30-8, NISHIJOUNAN 5-CHOME, OYAMA-SHI, TOCHIGI 323-0820 JAPAN.
2	TANAKAKIYOAKI	B102, 5932, TOMONUMA, NOGI-MACHI, SHIMOTSUGA-GUN, TOCHIGI 329-0101 JAPAN.
3	KURIYAMA KAZUHIKO	7-16, OTOME 1-CHOME, OYAMA-SHI, TOCHIGI 329-0214 JAPAN.
4	HORI WATARU	12-9 UTSUKUSHIGAOKA 3-CHOME, OYAMAS-SHI, TOCHIGI 329-0207 JAPAN.

PCT International Classification Number

A61K 31/661

PCT International Application Number

PCT/JP2004/001783

PCT International Filing date

2004-02-18

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1	2003-039269	2003-02-18	Japan